Atorvastatin - instructions for use, reviews, analogs and formulations (tablets 10 mg, 20 mg, 40 mg and 80 mg of Teva and Lexm) of a statin drug for reducing blood cholesterol levels in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Atorvastatin. Presented are reviews of visitors to the site - consumers of this medication, as well as the opinions of doctors specialists on the use of Atorvastatin in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Atorvastatin in the presence of existing structural analogues. The use of statin to lower blood cholesterol levels in adults, children,as well as during pregnancy and lactation. Composition of the preparation.

Atorvastatin - a hypolipidemic agent from the group of statins. A selective competitive inhibitor of HMG-CoA reductase, an enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A into mevalonic acid, a precursor of sterols, including cholesterol. Triglycerides (TG) and cholesterol in the liver are included in the composition of very low density lipoproteins (VLDL), enter the blood plasma and transport to peripheral tissues. Low density lipoproteins (LDL) are formed from VLDL in the course of interaction with LDL receptors. Atorvastatin lowers cholesterol and lipoprotein concentrations in the blood plasma, inhibiting HMG-CoA reductase, the synthesis of cholesterol in the liver, and an increase in the number of "liver" LDL receptors on the cell surface, which leads to increased capture and catabolism of LDL. Reduces the formation of LDL, causes a pronounced and persistent increase in the activity of LDL receptors. Reduces the concentration of LDL in patients with homozygous seminal hypercholesterolemia, which usually does not respond to lipid-lowering drugs.Reduces the concentration of total cholesterol by 30-46%, LDL by 41-61%, apolipoprotein B by 34-50% and TG by 14-33%; causes an increase in the concentration of HDL cholesterol (high-density lipoprotein) and apolipoprotein A. Dose-dependent lowers the concentration of LDL in patients with homozygous hereditary hypercholesterolemia resistant to therapy with other lipid-lowering drugs.

Composition

Atorvastatin calcium trihydrate + excipients.

Pharmacokinetics

Absorption is high. Food slightly reduces the speed and duration of absorption of the drug (by 25% and 9%, respectively), but the reduction in LDL cholesterol is similar to that of Atorvastatin without food. The concentration of atorvastatin when used in the evening is lower than in the morning (about 30%). A linear relationship between the degree of absorption and the dose of the drug has been revealed. Metabolized mainly in the liver under the action of the isoenzyme CYP3A4 with the formation of pharmacologically active metabolites (ortho- and parahydroxylated derivatives, beta-oxidation products). It is excreted with bile after hepatic and / or extrahepatic metabolism (it does not undergo significant intestinal hepatic recirculation).Less than 2% of the dose taken internally is determined in the urine. It is not excreted during hemodialysis.

Indications

• in combination with a diet to reduce the elevated concentrations of total cholesterol, cholesterol / LDL, apolipoprotein B and triglycerides, and increase HDL cholesterol in patients with primary hypercholesterolemia, heterozygous familial and non-family hypercholesterolemia, and combined hyperlipidemia (types 2a and 2b according to Fredrickson);
• in combination with a diet for the treatment of patients with elevated serum concentrations of triglycerides (type 4 according to Fredrickson) and patients with disbetalipoproteinemia (type 3 according to Fredrickson), in which diet therapy does not give an adequate effect;
• to reduce the concentration of total cholesterol and cholesterol / LDL in patients with homozygous familial hypercholesterolemia, when dietetics and other non-pharmacological treatments are not effective enough.

Forms of release

Tablets coated with 10 mg, 20 mg, 40 mg and 80 mg.

Instructions for use and dosage

Before the appointment of atorvastatin, the patient should be recommended a standard lipid-lowering diet, which he must comply with throughout the treatment period.

The drug can be taken at any time of the day with food or whatever time it takes to eat. The dose is selected taking into account the baseline levels of LDL-C, the purpose of therapy and the individual effect. At the beginning of treatment and / or during an increase in the dose of Atorvastatin, it is necessary to monitor the levels of lipids in the blood plasma every 2-4 weeks and adjust the dose accordingly.

The initial dose is on the average 10 mg 1 time per day and further varies from 10 mg to 80 mg once a day.

When administered simultaneously with cyclosporine, the daily dose of atorvastatin should not exceed 10 mg.

With primary hypercholesterolemia and mixed hyperlipidemia, when the serum level of TG (type 4 by Fredrickson) is increased, as well as with disbetalipoproteinemia (type 3 according to Fredrickson), in most cases it is sufficient to prescribe the drug at a dose of 10 mg once a day. A significant therapeutic effect is observed, usually after 2 weeks, the maximum therapeutic effect is usually observed after 4 weeks. With prolonged treatment, this effect persists.

With homozygous familial hypercholesterolemia, the drug is prescribed in a dose of 80 mg (4 tablets of 20 mg) once a day.

In patients with renal insufficiency and kidney disease, the concentration of atorvastatin in the blood plasma does not change, the degree of decrease in the level of LDL-C is preserved, therefore a change in the dose of the drug is not required.

With liver failure, the dose should be reduced.

When using the drug in elderly patients, there were no differences in safety, effectiveness, or achievement of lipid-lowering therapy goals in comparison with the general population.

Side effect

• insomnia;
• dizziness;
• headache;
• asthenia;
• malaise;
• drowsiness;
• nightmarish dreams;
• amnesia;
• emotional lability;
• paralysis of the facial nerve;
• migraine;
• depression;
• loss of consciousness;
• tinnitus;
• dryness of the conjunctiva;
• violation of accommodation;
• hemorrhage into the retina of the eye;
• deafness;
• glaucoma;
• loss of taste;
• chest pain;
• palpitation;
• orthostatic hypotension;
• increased blood pressure;
• phlebitis;
• arrhythmia;
• angina pectoris;
• anemia, thrombocytopenia;
• bronchitis;
• rhinitis;
• pneumonia;
• exacerbation of bronchial asthma;
• nose bleed;
• nausea, vomiting;
• heartburn;
• constipation or diarrhea;
• flatulence;
• abdominal pain;
• decreased or increased appetite;
• dry mouth;
• eructation;
• stomatitis;
• esophagitis;
• glossitis;
• gastroenteritis;
• cheilitis;
• duodenal ulcer;
• rectal bleeding;
• bleeding gums;
• arthritis;
• leg cramps;
• myositis;
• myalgia;
• rhabdomyolysis;
• torticollis;
• swelling of the joints;
• urogenital infections;
• peripheral edema;
• dysuria (including pollakiuria, nocturia, urinary incontinence or urinary retention, mandatory urges to urinate);
• leukocyturia, hematuria;
• decreased libido;
• impotence;
• violation of ejaculation;
• alopecia;
• photosensitization;
• increased sweating;
• eczema;
• seborrhea;
• gynecomastia;
• increase in body weight;
• exacerbation of gout;
• itching;
• skin rash;
• contact dermatitis;
• hives;
• angioedema;
• swelling of the face;
• anaphylaxis;
• multi-form exudative erythema (including Stevens-Johnson syndrome);
• toxic epidermal necrolysis (Lyell's syndrome).

Contraindications

• active liver disease;
• an increase in the activity of hepatic enzymes of unknown origin (more than 3-fold as compared with VGN);
• hepatic insufficiency (classes A and B on the Child-Pugh scale);
• pregnancy;
• lactation period;
• age under 18 years (effectiveness and safety not established);
• hypersensitivity to the components of the drug.

Application in pregnancy and lactation

Atorvastatin is contraindicated in pregnancy and lactation (breastfeeding).

It is not known whether atorvastatin is excreted in breast milk. Given the potential for adverse effects in infants, if necessary, use during lactation should decide the issue of termination of breastfeeding.

Women of reproductive age during treatment should use adequate methods of contraception. Atorvastatin can be administered to women of childbearing age only when the probability of pregnancy are very low and the patient informed of the potential risk of treatment to the fetus.

Use in children

Contraindicated in children and adolescents under the age of 18 years (efficacy and safety not established).

special instructions

Before starting therapy with atorvastatin, it is necessary to try to achieve control of hypercholesterolemia by adequate diet therapy, increased physical activity, weight loss in obese patients and treatment of other conditions.The hypocholesterolemic diet should be observed by patients during the entire treatment period.

The use of HMG-CoA reductase inhibitors to reduce lipid levels in the blood can lead to a change in biochemical indicators that reflect liver function. The liver function should be monitored before the start of therapy, 6 weeks, 12 weeks after the initiation of atorvastatin and after each dose increase, and periodically, for example, every 6 months. Increased activity of hepatic enzymes in blood serum can be observed during therapy with Atorvastatin. In such cases, patients should be monitored prior to the normalization of hepatic enzyme activity. If ALT or ACT values ​​are more than 3 times higher than ULN, it is recommended to reduce the dose of atorvastatin or discontinue treatment. Active liver disease or persistent increase in the activity of aminotransferases of unknown origin serve as contraindications to the administration of atorvastatin.

Treatment with atorvastatin may cause myopathy. In patients with common myalgia, tenderness or weakness of the muscles and / or a marked increase in the activity of CKK, there is a possibility of myopathy (pain and weakness in muscles, combined with an increase in CKK activity by more than 10 times compared with HHV).Therapy with Atorvastatin should be discontinued in the event of a marked increase in the activity of CKK or in the presence of confirmed or suspected myopathy. The risk of myopathy in treatment with other drugs of this class was increased with the simultaneous use of cyclosporine, fibrates, erythromycin, nicotinic acid or azole antifungal agents. Many of these drugs inhibit the metabolism mediated by the CYP3A4 isoenzyme and / or drug transport. Atorvastatin is biotransformed by the action of CYP3A4. When prescribing atorvastatin in combination with fibrates, erythromycin, immunosuppressants, azole antifungal agents, or nicotinic acid in hypolipidemic doses, the expected benefit and risk of treatment should be carefully weighed and patients monitored regularly to identify pain or weakness in the muscles, especially during the first months of treatment and in periods of increasing the dose of any drug. In such situations, it is possible to recommend a periodic determination of the activity of CKK, although such control does not prevent the development of severe myopathy.

When using Atorvastatin, as well as other drugs of this class, cases of rhabdomyolysis with acute renal failure due to myoglobinuria are described. Atorvastatin should be temporarily discontinued or completely discontinued if there is evidence of possible myopathy or the presence of a risk factor for developing renal failure against rhabdomyolysis (eg, severe acute infection, arterial hypotension, severe surgery, trauma, severe metabolic, endocrine and electrolyte disturbances and uncontrolled convulsions).

Patients should be warned that they should immediately consult a doctor if unexplained pain or weakness in the muscles occurs, especially if they experience malaise or fever.

Impact on the ability to drive vehicles and manage mechanisms

When driving vehicles or working with mechanisms, patients must be careful, since When using Atorvastatin, there is a risk of dizziness.

Drug Interactions

With the simultaneous use of atorvastatin with cyclosporine,inhibitors of HIV protease (indinavir, ritonavir), antibiotics (erythromycin, clarithromycin, quinupristin / dalfopristin), antifungal drugs from the azole group (fluconazole, itraconazole, ketoconazole), nefazodone, fibrolic acid derivatives, nicotinic acid or diltiazem, the concentration of atorvastatin in plasma increases, which increases the risk of myopathy with rhabdomyolysis and acute renal failure.

With simultaneous ingestion of atorvastatin and a suspension containing magnesium hydroxide and aluminum hydroxide, the concentration of atorvastatin in the blood plasma decreased by approximately 35%, but the degree of decrease in the level of LDL-C was not changed.

With the simultaneous use of Atorvastatin does not affect the pharmacokinetics of antipyrine (phenazone), therefore interaction with other agents metabolized by the same isoenzymes of the cytochrome P450 system is not expected.

With the simultaneous use of colestipol, the concentration of atorvastatin in the blood plasma is reduced by about 25%. However, the hypolipidemic effect of the combination of atorvastatin and colestipol was superior to that of each drug alone.

At repeated reception of Digoxin and Atorvastatinum in a dose of 10 mg Css digoxinum in a blood plasma did not vary.However, when using digoxin in combination with Atorvastatin 80 mg / day, the digoxin concentration increased by about 20%. When this combination is used, patients should be monitored.

With the simultaneous use of atorvastatin and Erythromycin (500 mg 4 times daily) or Clarithromycin (500 mg twice daily) that inhibit the isoenzyme CYP3A4, an increase in the concentration of atorvastatin in the blood plasma was observed.

With the simultaneous use of atorvastatin (10 mg once a day) and Azithromycin (500 mg once a day), the concentration of atorvastatin in the blood plasma did not change.

Atorvastatin did not have a clinically significant effect on the concentration of terfenadine in the blood plasma, which is metabolized mainly with the participation of CYP3A4; in this connection, it seems unlikely that atorvastatin can significantly affect the pharmacokinetic parameters of other substrates of the CYP3A4 isoenzyme.

With the simultaneous use of atorvastatin and an oral contraceptive containing norethindrone and ethinylestradiol, there was a significant increase in the AUC of norethindrone and ethinylestradiol by approximately 30% and 20%, respectively.This effect should be considered when choosing an oral contraceptive for a woman receiving atorvastatin.

Simultaneous use with drugs that reduce the concentration of endogenous steroid hormones (including cimetidine, ketoconazole, spironolactone) increases the risk of reducing endogenous steroid hormones (these combinations require caution).

When studying the interaction of atorvastatin with Warfarin and cimetidine, no signs of clinically significant interaction were found.

With the simultaneous use of atorvastatin in a dose of 80 mg and Amlodipine at a dose of 10 mg, the pharmacokinetics of atorvastatin did not change in the equilibrium state.

No clinically significant adverse effects of atorvastatin and antihypertensive agents have been observed.

The simultaneous use of atorvastatin with protease inhibitors, known as inhibitors of CYP3A4 (grapefruit juice), was accompanied by an increase in the concentration of atorvastatin in blood plasma, therefore, the use of this juice should be avoided.

Simultaneous use of atorvastatin with inducers of the isoenzyme CYP3A4 (efavirenz, rifampicin) leads to a decrease in the concentration of atorvastatin with blood plasma.

Pharmaceutical incompatibility is not known.

Analogues of the drug Atorvastatin

Structural analogs for the active substance:

• Anistat;
• Atokord;
• Atomax;
• Atorvastatin LEXM;
• Atorvastatin Teva;
• Atorvox;
• Atoris;
• The Vasator;
• Lipon;
• Lipofford;
• Liprimar;
• Liptonorm;
• TG tor;
• Torvazine;
• Torvacard;
• Tulip.

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